Pharmacokinetics, safety and tolerability of an oral suspension of fexofenadine for children with allergic rhinitis

Abstract

Allergic rhinitis (AR) is a common chronic condition in children and may impact a child's quality of life. Increasing treatment compliance may improve quality of life. An oral suspension of fexofenadine hydrochloride (HCl) has been developed to ease administration to children and may, therefore, improve treatment compliance. The purpose of this study was to assess the pharmacokinetic behavior, safety, and tolerability of a single dose of fexofenadine HCl oral suspension administered to children aged 2-5 years with allergic rhinitis. Children (aged 2-5 years) with AR were recruited in a multicenter, open-label, single-dose study. Fexofenadine HCl (30 mg) was administered as a 6-mg/mL suspension (5 mL). Plasma samples were collected up to 24 hours postdose. Adverse events (AEs); electrocardiograms (ECGs); vital signs; and clinical laboratory tests for hematology, blood chemistry, and urinalysis were analyzed to evaluate safety and tolerability. Fifty subjects completed the study. Mean maximum plasma concentration of fexofenadine was 224 ng/mL, and mean area under the plasma concentration curve was 898 ng . hour/mL. Treatment-emergent AEs were mild in intensity and reported in a total of seven subjects. No trends or clinically meaningful changes in mean ECG, vital sign, or clinical laboratory test data occurred during the study. In children aged 2-5 years, the exposure after a 30-mg dose of fexofenadine HCl suspension was similar to the exposures previously seen after a 30- and 60-mg dose of fexofenadine HCl in children aged 6-11 years and in adults, respectively. The suspension was also well tolerated.

Fexofenadine: review of safety, efficacy and unmet needs in children with allergic rhinitis

“…The oral suspension of fexofenadine (30 mg, twice daily) is recommended for the treatment of seasonal AR in children aged 2–11 years. For children > 6 years, an oral tablet of fexofenadine is available [ 18 , 50 , 51 ].…”

Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy

“…In children 2 to 5 years old with AR, oral suspension of fexofenadine was shown to be effective and safe in a multicenter, openlabel, single-dose study [24]. The safety of fexofenadine has been demonstrated in many studies that have shown it to be free from psychomotor adverse effects and free from sedation, even at greater-than-recommended doses.…”

The clinical evidence of second-generation H1-antihistamines in the treatment of allergic rhinitis and urticaria in children over 2 years with a special focus on rupatadine

“…Regarding the efficacy of antihistamines in the management of CSU in children there are also very limited data (Table 2) [34][35][36][37][38][39][40][41][42][43][44][45][46][47][48][49][50]. It is very noticeable that clinical efficacy studies have not been conducted with ebastine, fexofenadine, levocetirizine, bilastine, or desloratadine in pediatric patients with CSU and only one single study assessed the use of cetirizine in children under the age of 6 [36].…”

“…There are some published studies that reported safety data of sgAH in pediatric patients treated with cetirizine [38], levocetirizine [39], desloratadine [40,41], fexofenadine [42,43], bilastine [45][46][47], or ebastine (Table 3) [48][49][50]. These safety studies in children with allergic rhinitis or urticaria, however, had a noncomparative open label design, or were prospective observational studies, without efficacy comparative evaluations.…”

“…Safety data of second generation antihistamines from clinical studies in newborns and children. N = 111(Bloom, 2004) N = 50(Segall, 2008) N=453 (N = 120(Bloom, 2004) N/A *ETAC study: Early Treatment of the Atopic Child 12-24 months (18 months long-term safety)[38]. ** EPAAC study: Early Prevention of Asthma in Atopic Children 12-24 months (18 months long-term safety)[39].…”